DERIVES DE BETA-LACTAME, LES COMPOSITIONS PHARMACEUTIQUES LES CONTENANT ET LEUR PROCEDE DE PREPARATION

• Main Author: REZSO BOGNAR, CSABA JASZBERENYI, ERZSEBET FARKAS, MARIA PUNYICZKY, FERENC HERNADI, KATALIN EKE ET ILONA PETRIKOVICS
• Format: Patent
• Language: French
• Published: 14.01.1983
• Subjects: CHEMISTRY; HETEROCYCLIC COMPOUNDS; HUMAN NECESSITIES; HYGIENE; MEDICAL OR VETERINARY SCIENCE; METALLURGY; ORGANIC CHEMISTRY; PREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES; SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS ORMEDICINAL PREPARATIONS

LES COMPOSES DE L'INVENTION REPONDENT A LA FORMULE GENERALE:(CF DESSIN DANS BOPI)DANS LAQUELLE NOTAMMENT:R EST DE L'HYDROGENE,A EST UN GROUPE DE LA FORMULE GENERALE A,R EST UN GROUPE PHENYLE,R ET R SONT DES ATOMES D'HYDROGENE,N ET T REPRESENTENT CHAQUE ZERO,X EST UN GROUPE DE LA FORMULE -CH-C(CH)-,Q EST UN ATOME D'OXYGENE. Ceph-3-em-4-carboxylic acid and 2,2-dimethyl-penam-3-carboxylic acid derivatives of the general formula (I), wherein: R R N- or R R -NR -, X is -C(CH3)2-, -CH2-C(CH3)= -CH2-C(CH2OAc)= or -CH2-C(CH2SHet)=, Het is a 5-7 membered heterocyclic group containing 1-4 nitrogen atom(s) and optionally one or more other hetero atom(s), optionally condensed with one or more phenyl group(s) and/or substituted with one or more alkyl, aralkyl, aryl, substituted aryl or substituted aralkyl group(s), R is hydrogen atom, a C1-4 alkyl group or a phenyl group bearing optionally a halo, hydroxy, alkoxy or alkyl substituent, R is hydrogen atom, a C1-4 alkyl group or a phenyl group bearing optionally a halo, hydroxy, alkoxy or alkyl substituent, R and R each stand for hydrogen atom, a C1-4 alkyl group or a phenyl group bearing optionally a halo, hydroxy, alkoxy or alkyl substituent, Q represents oxygen, sulfur or selenium atom, R is hydrogen atom, a C1-4 alkyl group or a group -COOR , R being a C1-8 alkyl group, a benzyl group, a benzhydryl group or a phenyl group bearing optionally a halo, hydroxy, alkoxy or alkyl substituent, R is a phenyl group bearing optionally one or more halo, C1-6 alkyl, nitro, alkoxycarbonyl, trifluoromethyl, dialkylamino, hydroxy, carboxylic acid or sulfonic acid substituent(s), a C1-8 alkyl group optionally bearing an alkoxycarbonyl, hydroxyl, dialkylamino or alkoxy substituent, a C3-8 cycloalkyl group, a C2-6 alkenyl group, a naphthyl group, a heteroaryl group, a 3-8 membered heterocyclyl group optionally condensed with one or more phenyl group(s) and/or bearing one or more substituent(s), or an adamantyl group, and R is hydrogen, or R and R form, together with the adjacent nitrogen atom, a 4-8 membered, unsubstituted or substituted heterocyclic group optionally containing one or more additional nitrogen, oxygen or sulfur atom(s) and optionally condensed with one or more phenyl ring(s), Z is hydroxy group, n is zero or one, and t is zero, one or two, and their pharmacologically acceptable salts and biologically active esters possess strong antimicrobial and enzyme inhibiting, particularly antibacterial and beta -lactamase inhibiting effects.